NOVEL EPOXYSUCCINYL PEPTIDES - SELECTIVE INHIBITORS OF CATHEPSIN-B, INVITRO
NOVEL EPOXYSUCCINYL PEPTIDES - SELECTIVE INHIBITORS OF CATHEPSIN-B, INVITRO
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DOI：
10.1016/0014-5793(91)80318-w
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发表时间：
1991-03-25
期刊：
影响因子：
3.5
通讯作者：
KATUNUMA, N
中科院分区：
文献类型：
--
作者：
MURATA, M;MIYASHITA, S;KATUNUMA, N
设计合成了一系列新的环氧琥珀酰基多肽来开发组织蛋白酶B的特异性抑制剂，其中N-(L-3-trans-ethoxycarbonyloxirane-2-carbonyl)-L-isoleucyl-L-proline(化合物CA-030)和N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-proline(化合物CA-074)是体外最有效、最特异的组织蛋白酶B抑制剂。组织蛋白酶B与其他半胱氨酸蛋白酶如组织蛋白酶L、组织蛋白酶H、组织蛋白酶H、组织蛋白酶L、组织蛋白酶H、组织蛋白酶等相比，组织蛋白酶B的羧基和乙酸乙酯基团或正丙胺基是必需的。
A series of new epoxysuccinyl peptides were designed and synthesized to develop a specific inhibitor of cathepsin B. Of these compounds, N-(L-3-trans-ethoxycarbonyloxirane-2-carbonyl)-L-isoleucyl-L-proline (compound CA-030) and N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-proline (compound CA-074) were the most potent and specific inhibitors of cathepsin B in vitro. The carboxyl group of proline and the ethyl ester group or n-propylamide group in the oxirane ring were necessary, the ethyl ester group or the n-propylamide group being particularly effective for distinguishing cathepsin B from other cysteine proteinases such as cathepsins L and H, and calpains.